CA2926596C - Compose heterocyclique condense, son procede de preparation, composition pharmaceutique et leurs utilisations - Google Patents

Compose heterocyclique condense, son procede de preparation, composition pharmaceutique et leurs utilisations Download PDF

Info

Publication number
CA2926596C
CA2926596C CA2926596A CA2926596A CA2926596C CA 2926596 C CA2926596 C CA 2926596C CA 2926596 A CA2926596 A CA 2926596A CA 2926596 A CA2926596 A CA 2926596A CA 2926596 C CA2926596 C CA 2926596C
Authority
CA
Canada
Prior art keywords
compound
synthesis
group
ring
hydrogen
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CA2926596A
Other languages
English (en)
Other versions
CA2926596A1 (fr
Inventor
Zusheng Xu
Yangtong Lou
Original Assignee
Shanghai Yingli Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Shanghai Yingli Pharmaceutical Co Ltd filed Critical Shanghai Yingli Pharmaceutical Co Ltd
Publication of CA2926596A1 publication Critical patent/CA2926596A1/fr
Application granted granted Critical
Publication of CA2926596C publication Critical patent/CA2926596C/fr
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

L'invention porte sur un composé hétérocyclique condensé, sur son procédé de préparation, sur une composition pharmaceutique et sur leurs utilisations. Le composé hétérocyclique condensé est représenté par la formule I, la formule II ou la formule III. Le procédé de préparation du composé hétérocyclique condensé et/ou du sel pharmaceutiquement acceptable de celui-ci selon la présente invention comporte trois voies de synthèse. La présente invention porte également sur une composition pharmaceutique du composé hétérocyclique condensé, la composition pharmaceutique contenant un ou plusieurs des composés hétérocycliques condensés, représentés par la formule I, la formule II ou la formule III, des sels pharmaceutiquement acceptables de ceux-ci, des hydrates, des solvates, des polymorphes et des promédicaments de ceux-ci, et un vecteur pharmaceutiquement acceptable. La présente invention porte également sur une application du composé hétérocyclique condensé et/ou de la composition pharmaceutique dans la préparation d'inhibiteurs de kinases et de médicaments pour la prévention et le traitement de maladies liées à une kinases. Le composé hétérocyclique condensé selon la présente invention possède une fonction d'inhibition sélective sur PI3Kd et peut être utilisé pour préparer des médicaments pour la prévention et le traitement de maladies caractérisées par une prolifération cellulaire telles que des cancers, des infections, des inflammations ou des maladies auto-immunes.
CA2926596A 2013-10-16 2014-09-19 Compose heterocyclique condense, son procede de preparation, composition pharmaceutique et leurs utilisations Active CA2926596C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201310485200 2013-10-16
CN201310485200.6 2013-10-16
PCT/CN2014/086914 WO2015055071A1 (fr) 2013-10-16 2014-09-19 Composé hétérocyclique condensé, son procédé de préparation, composition pharmaceutique et leurs utilisations

Publications (2)

Publication Number Publication Date
CA2926596A1 CA2926596A1 (fr) 2015-04-23
CA2926596C true CA2926596C (fr) 2020-07-14

Family

ID=52827649

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2926596A Active CA2926596C (fr) 2013-10-16 2014-09-19 Compose heterocyclique condense, son procede de preparation, composition pharmaceutique et leurs utilisations

Country Status (14)

Country Link
US (1) US9656996B2 (fr)
EP (1) EP3059238B1 (fr)
JP (1) JP6139789B2 (fr)
KR (1) KR101982912B1 (fr)
CN (3) CN106831722B (fr)
AU (1) AU2014336775B2 (fr)
CA (1) CA2926596C (fr)
IL (1) IL245112B (fr)
MX (1) MX381304B (fr)
NZ (1) NZ718487A (fr)
RU (1) RU2663999C2 (fr)
SG (1) SG11201602446VA (fr)
TW (1) TWI631115B (fr)
WO (1) WO2015055071A1 (fr)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2926596C (fr) 2013-10-16 2020-07-14 Shanghai Yingli Pharmaceutical Co., Ltd Compose heterocyclique condense, son procede de preparation, composition pharmaceutique et leurs utilisations
US10765681B2 (en) 2016-02-05 2020-09-08 Academia Sinica Purine compounds possessing anticancer activity
HRP20210508T1 (hr) * 2016-06-16 2021-05-28 Janssen Pharmaceutica Nv Biciklički derivati piridina, pirazina i pirimidina kao inhibitori pi3k beta
EA201992296A1 (ru) 2017-03-29 2020-02-12 Янссен Фармацевтика Нв Производные хиноксалина и пиридопиразина в качестве ингибиторов pi3k-бета
US11760701B2 (en) 2018-02-27 2023-09-19 The Research Foundation For The State University Of New Yrok Difluoromethoxylation and trifluoromethoxylation compositions and methods for synthesizing same
SG11202103118PA (en) 2018-09-27 2021-04-29 Shanghai Yingli Pharmaceutical Co Ltd Crystal form of morpholino quinazoline compound, preparation method therefor and use thereof
KR102405055B1 (ko) * 2019-01-16 2022-06-07 상하이 잉리 파마슈티컬 컴퍼니 리미티드 모르폴리노퀴나졸린 화합물의 제조방법 및 이의 중간체
CN111848598B (zh) * 2019-04-26 2024-12-10 健艾仕生物医药有限公司 一种含杂环的化合物、其应用及含其的组合物
CN111943938A (zh) * 2019-05-17 2020-11-17 上海再极医药科技有限公司 一种a2a腺苷受体拮抗剂的合成方法
KR102803409B1 (ko) 2019-06-06 2025-05-07 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 Atr 키나제 억제제로서의 2,4,6-삼치환된 피리미딘 화합물
KR20220140515A (ko) 2020-01-13 2022-10-18 버지 애널리틱스, 인크. 치환된 피라졸로-피리미딘 및 그의 용도
CN113444073B (zh) * 2020-03-26 2024-01-05 上海璎黎药业有限公司 吗啉基喹唑啉类化合物的晶型ⅲ、其制备方法及应用
CN115120732B (zh) * 2021-03-26 2025-05-30 上海璎黎药业有限公司 一种喹唑啉化合物的药物组合物及其制备方法
CN115120596A (zh) * 2021-03-26 2022-09-30 上海璎黎药业有限公司 一种喹唑啉化合物及药物组合物的应用
WO2022228218A1 (fr) * 2021-04-30 2022-11-03 上海璎黎药业有限公司 Application d'un composé quinazoline et composition pharmaceutique
WO2022247770A1 (fr) * 2021-05-24 2022-12-01 上海璎黎药业有限公司 Composé hétérocyclique contenant de l'azote, son procédé de préparation et son application
CN118139626A (zh) * 2021-09-01 2024-06-04 江苏恒瑞医药股份有限公司 一种pi3k抑制剂与btk抑制剂在制备治疗淋巴瘤的药物中的用途
CN116693519A (zh) 2022-03-04 2023-09-05 上海璎黎药业有限公司 一种含五元杂芳环结构化合物、其药物组合物及应用
CN118525011A (zh) * 2022-08-24 2024-08-20 上海璎黎药业有限公司 一种吗啉基喹唑啉类化合物、其制备方法及应用

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY141144A (en) 2000-03-02 2010-03-15 Smithkline Beecham Corp 1, 5-disubstituted-3,4-dihydro-1h-pyrimido 4,5-dipyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
US7235551B2 (en) 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
CN100345830C (zh) * 2000-04-27 2007-10-31 安斯泰来制药有限公司 稠合杂芳基衍生物
EP1608652A1 (fr) 2003-03-31 2005-12-28 Vernalis (Cambridge) Limited Composes pyrazolopyrimidines et leur utilisation en medecine
EP1653969A4 (fr) * 2003-08-07 2006-12-20 Japan Tobacco Inc Derives de pyrrolo 1,2-b pyridazine
EP1819342A4 (fr) 2004-12-03 2008-12-17 Merck & Co Inc Antagonistes de récepteurs de tachykinine de type quinoline
ES2513165T3 (es) 2005-10-07 2014-10-24 Exelixis, Inc. Derivados de N-(3-amino-quinoxalin-2-il)-sulfonamida y su uso como inhibidores de la fosfatidilinositol-3-quinasa
NL2000323C2 (nl) 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
MX2008013583A (es) 2006-04-26 2008-10-31 Genentech Inc Compuestos del inhibidor de fosfoinositido 3-cinasa y composiciones farmaceuticas que los contienen.
KR101533461B1 (ko) 2006-04-26 2015-07-02 에프. 호프만-라 로슈 아게 Ｐｉ３ｋ저해제로 유용한 티에노［3,2-ｄ］피리미딘 유도체
BRPI0714908B8 (pt) 2006-08-08 2021-05-25 Chugai Pharmaceutical Co Ltd derivados de pirimidina como inibidor de pi3k, composição farmacêutica e agente preventivo ou agente terapêutico de uma doença proliferativa que os compreende
CN102336752A (zh) 2006-11-20 2012-02-01 诺瓦提斯公司 2-甲基-2-[4-(3-甲基-2-氧代-8-喹啉-3-基-2,3-二氢-咪唑并[4,5-c]喹啉-1-基)-苯基]-丙腈的盐和晶型
NZ580009A (en) 2007-04-11 2012-06-29 Exelixis Inc Combination therapies comprising quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer
WO2008152387A1 (fr) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Dérivés de quinazoline comme inhibiteurs de pi3 kinase
JP5736171B2 (ja) * 2007-09-24 2015-06-17 ジェネンテック， インコーポレイテッド チアゾロピリミジンｐｉ３ｋ阻害剤化合物および使用方法
WO2009045174A1 (fr) * 2007-10-05 2009-04-09 S*Bio Pte Ltd 2 -morpholinylpurines en tant qu'inhibiteurs de pi3k
CN104119336B (zh) * 2007-10-05 2016-08-24 维拉斯通股份有限公司 嘧啶取代的嘌呤衍生物
TW200938201A (en) * 2008-02-07 2009-09-16 Chugai Pharmaceutical Co Ltd Pyrrolopyrimidine derivative as PI3K inhibitor and use thereof
CA2721851A1 (fr) * 2008-05-30 2009-12-03 Genentech, Inc. Composes inhibiteurs de la pi3k de type purine et procedes d'utilisation
ES2566339T3 (es) 2008-06-05 2016-04-12 Glaxo Group Limited Derivados de 4-carboxamida indazol útiles como inhibidores de PI3-quinasas
JP5502077B2 (ja) 2008-06-05 2014-05-28 グラクソ グループ リミテッド 新規な化合物
CA2730271A1 (fr) * 2008-07-07 2010-01-14 Xcovery Holding Company Llc Inhibiteurs selectifs des isoformes de la pi3 kinase
US8586582B2 (en) 2008-11-11 2013-11-19 Xcovery Holding Company, Llc PI3K/mTOR kinase inhibitors
AU2010213192A1 (en) 2009-02-13 2011-08-04 Bayer Intellectual Property Gmbh Fused pyrimidines
WO2010114494A1 (fr) * 2009-04-03 2010-10-07 S*Bio Pte Ltd Purines 2-morpholino 8-substituées pour une utilisation en tant qu'inhibiteurs de pi3k et/ou mtor dans le traitement de troubles prolifératifs
JP5465318B2 (ja) 2009-04-03 2014-04-09 ベラステム・インコーポレーテッド キナーゼ阻害剤としてのピリミジン置換プリン化合物
WO2010120987A1 (fr) 2009-04-17 2010-10-21 Wyeth Llc Composés de morpholino-pyrimidine à pont uréidoaryle et carbamoylaryle, à cycles condensés, leur utilisation en tant qu'inhibiteurs de kinase mtor et de kinase pi3, et leurs synthèses
WO2010120994A2 (fr) * 2009-04-17 2010-10-21 Wyeth Llc Composés d'uréido-aryl-pyrimidine et de carbamoylaryl-morpholino-pyrimidine, leur utilisation comme inhibiteurs de la kinase mtor et de la kinase pi-3, et leur synthèse
JP2012531436A (ja) * 2009-06-25 2012-12-10 アムジエン・インコーポレーテツド 複素環式化合物およびそれらのｐｉ３ｋ活性阻害剤としての使用
WO2011041399A2 (fr) 2009-09-29 2011-04-07 Tyrogenex, Inc. Inhibiteurs sélectifs de la pi3k (delta)
DE102009049679A1 (de) * 2009-10-19 2011-04-21 Merck Patent Gmbh Pyrazolopyrimidinderivate
AR079814A1 (es) * 2009-12-31 2012-02-22 Otsuka Pharma Co Ltd Compuestos heterociclicos, composiciones farmaceuticas que los contienen y sus usos
EP2539337A1 (fr) 2010-02-22 2013-01-02 F. Hoffmann-La Roche AG Composés de pyrido[3,2-d]pyrimidine inhibiteurs de pi3k delta et procédés d'utilisation
AU2011256195A1 (en) * 2010-05-19 2012-12-06 Xcovery Holding Company, Llc. mTOR selective kinase inhibitors
CA2802808A1 (fr) 2010-07-14 2012-01-19 F. Hoffmann-La Roche Ag Composes de purine selectifs de la pi3k p110 delta, et procedes d'utilisation
JP5965402B2 (ja) 2010-09-08 2016-08-03 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｎ−［５−［４−（５−｛［（２ｒ，６ｓ）−２，６−ジメチル−４−モルホリニル］メチル｝−１，３−オキサゾール−２−イル）−１ｈ−インダゾール−６−イル］−２−（メチルオキシ）−３−ピリジニル］メタンスルホンアミドの多形体および塩
WO2012032065A1 (fr) 2010-09-08 2012-03-15 Glaxo Group Limited Dérivés indazole à utiliser dans le traitement d'une infection par le virus de la grippe
JP5954838B2 (ja) 2010-09-14 2016-07-20 エクセリクシス， インク． Ｐｉ３ｋ−デルタの阻害剤ならびにそれらの使用法および製造法
US20130324561A1 (en) 2010-09-24 2013-12-05 Gilead Calistroga Llc. Atropisomers of p13k-inhibiting compounds
CA2813333C (fr) * 2010-10-01 2019-01-15 Novartis Ag Procede de fabrication de derives de pyrimidine
EP3170813B1 (fr) * 2010-10-06 2018-12-12 GlaxoSmithKline LLC Dérivés de benzimidazole comme inhibiteurs de pi3 kinase
CA2831582C (fr) 2011-03-28 2019-01-08 Mei Pharma, Inc. (aralkylamino et heteroarylalkylamino alpha-substitues)pyrimidinyl- et 1,3,5-triazinylbenzimidazoles, compositions pharmaceutiques associees etleur utilisation dans le traitement de maladies proliferatives
US20140163023A1 (en) * 2011-04-04 2014-06-12 Cellzome Limited Dihydropyrrolo pyrimidine derivatives as mtor inhibitors
US20130123255A1 (en) 2011-11-10 2013-05-16 Chugai Seiyaku Kabushiki Kaisha Combination of a pi3k inhibitor and a mek inhibitor
FR2986232B1 (fr) * 2012-01-26 2014-02-14 Sanofi Sa Derives heterocycliques bicycliques, leur preparation et leur application en therapeutique
US9499561B2 (en) 2012-04-10 2016-11-22 Shanghai Yingli Pharmaceutical Co., Ltd. Fused pyrimidine compound, and preparation method, intermediate, composition, and uses thereof
CA2926596C (fr) 2013-10-16 2020-07-14 Shanghai Yingli Pharmaceutical Co., Ltd Compose heterocyclique condense, son procede de preparation, composition pharmaceutique et leurs utilisations

Also Published As

Publication number Publication date
CN106831721B (zh) 2019-10-22
EP3059238B1 (fr) 2020-05-27
CN106831722A (zh) 2017-06-13
CN106831722B (zh) 2019-08-30
AU2014336775B2 (en) 2018-04-05
KR20160062170A (ko) 2016-06-01
NZ718487A (en) 2020-01-31
CN104557872A (zh) 2015-04-29
KR101982912B1 (ko) 2019-09-10
WO2015055071A1 (fr) 2015-04-23
CA2926596A1 (fr) 2015-04-23
TW201518288A (zh) 2015-05-16
SG11201602446VA (en) 2016-05-30
RU2016115934A (ru) 2017-11-20
JP2016533372A (ja) 2016-10-27
RU2663999C2 (ru) 2018-08-14
MX2016004964A (es) 2016-07-11
CN104557872B (zh) 2017-05-24
US20160244432A1 (en) 2016-08-25
MX381304B (es) 2025-03-12
EP3059238A1 (fr) 2016-08-24
TWI631115B (zh) 2018-08-01
JP6139789B2 (ja) 2017-05-31
US9656996B2 (en) 2017-05-23
AU2014336775A1 (en) 2016-04-21
CN106831721A (zh) 2017-06-13
IL245112B (en) 2020-10-29
IL245112A0 (en) 2016-06-30
EP3059238A4 (fr) 2017-04-12
HK1209738A1 (en) 2016-04-08

Similar Documents

Publication Publication Date Title
CA2926596C (fr) Compose heterocyclique condense, son procede de preparation, composition pharmaceutique et leurs utilisations
CA2904641C (fr) Inhibiteurs d'adn-pk
CN114845711B (zh) Raf激酶的抑制剂
AU2021208025A1 (en) Pyrimidine-4(3H)-ketone heterocyclic compound, preparation method therefor and use thereof in medicine and pharmacology
US20230118795A1 (en) Aryl or heteroaryl pyridone or pyrimidine derivative, preparation method and use thereof
JP2021513530A (ja) テトラヒドロイソキノリン化合物、その調製方法、そのような化合物を含む医薬組成物およびその使用
EP3277683B1 (fr) Derives tricycliques de 1-(cyclo)alkylpyridin-2-one condensee utiles dans le traitement du cancer
CN114929707B (zh) Eed抑制剂及其制备方法和用途
WO2024102621A1 (fr) Modulateurs de akt1
CA3004534A1 (fr) Pyrimidines fusionnees utilisees comme inhibiteurs de la phosphoinositide 3-kinase alpha selectifs d'une isoforme et leur procede de preparation
WO2024212024A1 (fr) Nouveaux composés pyrrole substitués, compositions comprenant le composé pyrrole substitué et leurs procédés d'utilisation
AU2023250757A1 (en) Heteroaryl derivative and use thereof
CA3158698A1 (fr) Bicycles a base de pyrimidine utilises en tant qu'agents antiviraux pour le traitement et la prevention d'une infection par le vih
AU2022272704A1 (en) Nitrogen-containing heterocyclic compound
WO2025011479A1 (fr) Inhibiteurs à base de pyrazole de ldh et leur utilisation dans des maladies immunitaires et inflammatoires
RU2807545C2 (ru) Тетразол-содержащие ингибиторы регулирующей апоптотические сигналы киназы 1 и способы их применения
CN117186093A (zh) PI3Kα变构抑制剂
CN116063325A (zh) 具有btk调节作用的大环化合物及其用途
HK1209738B (en) Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof
NZ712576B2 (en) Dna-pk inhibitors

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20160406

MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 10TH ANNIV.) - STANDARD

Year of fee payment: 10

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20240829

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20240829